Enhancement of the in vitro skin permeability of azidothymidine (AZT) via iontophoresis and chemical enhancer.
Azidothymidine (AZT) was used as a model drug to study the effect of iontophoresis on the skin permeation of a neutral compound. The rate of in vitro permeation across hairless rat skin was low and highly variable. With iontophoresis treatment the permeation rate was two- to threefold greater than by passive diffusion. The addition of varying amounts of sodium chloride to the donor enhanced the iontophoretic permeation rate an additional two- to threefold possibly due to convective forces. The addition of N-decylmethyl sulfoxide (C10MSO) to the donor increased the permeation rate by several hundred-fold over passive diffusion for hairless rat skin and approximately 75-fold for human skin. No additional enhancement was observed with the combination of C10MSO and iontophoresis treatment at constant current or constant voltage. It may be that the presence of C10MSO lowers the zeta potential of the skin, thus enhancement due to convective flow is minimized.
Wearley
L
L
Controlled Drug-Delivery Research Center, College of Pharmacy, Rutgers State University, Piscataway, New Jersey 08855-0789.
Chien
Y W
YW
D000818:Animals; D004058:Diffusion; D004121:Dimethyl Sulfoxide / Q000494:pharmacology / Q000031:analogs & derivatives; D004558:Electric Stimulation; D005079:Excipients; D006801:Humans; D066298:In Vitro Techniques; D007478:Iontophoresis; D008297:Male; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects; D012879:Skin Physiological Phenomena; D015215:Zidovudine / Q000008:administration & dosage / Q000493:pharmacokinetics*
D005079:Excipients; C054274:1-decyl methyl sulfoxide; D015215:Zidovudine; D004121:Dimethyl Sulfoxide